Impact of Biorelevant Media on Apparent Solubility and Biopharmaceutical Classification of Poorly Soluble Compounds

Purpose.  The goal of this study was to measure the apparent solubility of a diverse series of poorly soluble compounds in four different biorelevant dissolution media (BDM, eg. FeSSIF, FaSSIF, and blanks for each) by simulating intestinal conditions to investigate the result in potential BCS classification.  The µDISS Profiler™ allowed simultaneous measurement of dissolution rate and solubility in small volumes of BDM.

Conclusion.  All seven compounds displayed higher solubility in FeSSIF than in the corresponding blank buffer. Increased solubility in the BDM resulted in an improved rating in the BCS for cinnarizine, felodipine, indomethacin, terfenadine from class II to class I.  Danazol and glibenclamide remained unchanged.